发布求助
文献互助 智能选刊 最新文献

Il Farmaco; edizione scientifica最新文献

筛选
英文 中文
[Analgesic activity of derivatives of 7-amino-2,3-polymethylenindoles and their congeners]. [7-氨基-2,3-聚亚甲基吲哚衍生物及其同系物的镇痛活性]。
Il Farmaco; edizione scientifica Pub Date : 1988-02-01
R Cerri, G Boatto, A Pau, F Sparatore, P Manca
{"title":"[Analgesic activity of derivatives of 7-amino-2,3-polymethylenindoles and their congeners].","authors":"R Cerri,&nbsp;G Boatto,&nbsp;A Pau,&nbsp;F Sparatore,&nbsp;P Manca","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Some N-trifluoromethylsulphonyl and N-trifluoroacetylderivatives of 7-amino-2,3-polymethyleneindoles and of 7-amino-3-propylindole [(I) - (XIII)] were prepared and tested, together with corresponding aniline derivates [(XIV) - (XIX)] and with N-trifluoromethylsulphonylcyclopentylamine (XX), against formic acid induced writhings in mice. With very few exceptions, at the oral dose of 0.167 mmole/kg, they proved from 2 to 3.4 times more active than acetanilide.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 2","pages":"113-23"},"PeriodicalIF":0.0,"publicationDate":"1988-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14517775","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Benzodiazepine receptor ligands. Synthesis and preliminary pharmacological evaluation of some 3-aryl-6-thioalkyl-, 3-aryl-6-alkylsulphinyl-, 3-aryl-6-alkylsulphonyl-, and 3-aryl-6-alkoxy-1,2,4-triazolo[3,4-a]phthalazines. 苯二氮卓类受体配体。一些3-芳基-6-硫代烷基-、3-芳基-6-烷基磺酰-、3-芳基-6-烷基磺酰-和3-芳基-6-烷氧基-1,2,4-三唑[3,4-a]苯酞的合成及初步药理评价。
Il Farmaco; edizione scientifica Pub Date : 1988-02-01
G Tarzia, E Occelli, N Corsico, F Luzzani, D Barone
{"title":"Benzodiazepine receptor ligands. Synthesis and preliminary pharmacological evaluation of some 3-aryl-6-thioalkyl-, 3-aryl-6-alkylsulphinyl-, 3-aryl-6-alkylsulphonyl-, and 3-aryl-6-alkoxy-1,2,4-triazolo[3,4-a]phthalazines.","authors":"G Tarzia,&nbsp;E Occelli,&nbsp;N Corsico,&nbsp;F Luzzani,&nbsp;D Barone","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A series of 3-aryl-6-alkoxy- and some 3-aryl-6-thioalkyl-, 3-aryl-6-alkylsulphinyl-, and 3-aryl-6-alkylsulphonyl-1,2,4-triazolo[3,4-a]phthalazines were synthesised and tested for inhibition of the in vitro binding of 3H-Diazepam to benzodiazepine receptors in membranes isolated from rat brain synaptosomes. 6-Alkoxy-3-(4'-methoxy)phenyl-1,2,4-triazolo[3,4-a]phthalazines were more active than or as active as diazepam in the binding assay (Ki nM) but unlike diazepam their binding to the benzodiazepine receptors was not enhanced by 4-aminobutyric acid. These compounds did not antagonize pentylenetetrazole induced convulsions and were inactive in modifying the conditioned behaviour of rats. Compound (II a) counteracted the muscle relaxant effects of diazepam (traction test). These results suggest that (II a) may be a benzodiazepine receptor antagonist.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 2","pages":"189-201"},"PeriodicalIF":0.0,"publicationDate":"1988-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13977457","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
New congeners of antihypertensive and antithrombotic 7-amino or 7-acetyl-aminosubstituted-4,4a-dihydro-5H-indeno (1,2-c)pyridazin-3-ones. 抗高血压和抗血栓的7-氨基或7-乙酰氨基取代-4,4 -二氢- 5h -吲哚(1,2-c)吡啶嗪-3-酮的新同源物。
Il Farmaco; edizione scientifica Pub Date : 1988-02-01
G Cignarella, D Barlocco, L Landriani, M Folloni, G A Pinna, F Sala, M Germini
{"title":"New congeners of antihypertensive and antithrombotic 7-amino or 7-acetyl-aminosubstituted-4,4a-dihydro-5H-indeno (1,2-c)pyridazin-3-ones.","authors":"G Cignarella,&nbsp;D Barlocco,&nbsp;L Landriani,&nbsp;M Folloni,&nbsp;G A Pinna,&nbsp;F Sala,&nbsp;M Germini","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>New congeners of the antihypertensive and antithrombotic 7-amino-(I b) and 7-acetylamino-4,4a-dihydro-5H-indeno(1,2-c)pyridazin-3-one (I c) have been synthesized and evaluated pharmacologically. Compounds (I k) (R = 7-NHCH3), (I l) (R = 7-N(CH3)COCH3) and (I m) (R = 7-N(CH3)COC2H5) exhibited an antihypertensive effect similar to that of (I b) and (I c), though short lasting. The antithrombotic activity of six compounds was found comparable to or higher than that of acetylsalicilic acid. In particular, (I l) and (I m) fully protected mice against thrombosis, as did the reference compound (I c).</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 2","pages":"169-79"},"PeriodicalIF":0.0,"publicationDate":"1988-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14517777","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
[Synthesis and pharmacologic study of several spirohydantoins: relation to conformation]. [几种螺旋藻毒素的合成及药理研究:与构象的关系]。
Il Farmaco; edizione scientifica Pub Date : 1988-02-01
J C Courtoison, P Coudert, J Couquelet, P Tronche, M Jonadet, P Bastide
{"title":"[Synthesis and pharmacologic study of several spirohydantoins: relation to conformation].","authors":"J C Courtoison,&nbsp;P Coudert,&nbsp;J Couquelet,&nbsp;P Tronche,&nbsp;M Jonadet,&nbsp;P Bastide","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Using two routes starting from cyclanones, it has been possible to prepare two series of spirohydantoins substituted or not on the hydantoin nucleus nitrogen. These compounds exhibited low toxicity on pig lens aldose reductase (except for two compounds). A discussion is given on the steric and geometric requirements for effective enzyme inhibiting activity.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 2","pages":"153-60"},"PeriodicalIF":0.0,"publicationDate":"1988-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14265660","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Dopamine receptor agonists: new angularly annulated tricyclic compounds. 多巴胺受体激动剂:新的角环三环化合物。
Il Farmaco; edizione scientifica Pub Date : 1988-01-01
R Perrone, F Berardi, G Bettoni, V Tortorella
{"title":"Dopamine receptor agonists: new angularly annulated tricyclic compounds.","authors":"R Perrone,&nbsp;F Berardi,&nbsp;G Bettoni,&nbsp;V Tortorella","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In order to study the influence on dopaminergic activity of the exchange of X in rigid dopamine congeners of structure 1, the synthesis of octahydrobenzo [f] trans-quinoxalines (VII c, d) and trans-hexahydro-4H-naphtho[1,2-b][1,4]thiazines (X c, d), is reported.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 1","pages":"61-9"},"PeriodicalIF":0.0,"publicationDate":"1988-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14521129","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Chemotherapeutic agents with an imidazole moiety. II. Synthesis and biological activities of new 1,4-diarylimidazoles. 含有咪唑基团的化疗药物。2新型1,4-二芳基咪唑的合成及生物活性研究。
Il Farmaco; edizione scientifica Pub Date : 1988-01-01
G C Porretta, F Cerreto, R Fioravanti, M Scalzo, M Fischetti, F Riccardi, A Capezzone de Joannon, G de Feo, G Mazzanti, L Tolu
{"title":"Chemotherapeutic agents with an imidazole moiety. II. Synthesis and biological activities of new 1,4-diarylimidazoles.","authors":"G C Porretta,&nbsp;F Cerreto,&nbsp;R Fioravanti,&nbsp;M Scalzo,&nbsp;M Fischetti,&nbsp;F Riccardi,&nbsp;A Capezzone de Joannon,&nbsp;G de Feo,&nbsp;G Mazzanti,&nbsp;L Tolu","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis, antifungal and pharmacological activities of new 1,4-diarylimidazoles are reported. Antimicrobial data in comparison with antifungal antibiotic pyrrolnitrin pointed out that the 1,4-diaryl-2-mercaptoimidazole derivatives were inactive and all 1,4-diarylimidazoles exhibited a weak antifungal activity. Some compounds showed a selective activity against strains of Candida sp. Instead pharmacological data did not evidence any significant antiinflammatory activity. The tested compounds were prepared by reacting appropriate phenacylanilines with potassium thiocyanate in acidic medium to afford 1,4-diaryl-2-mercapto imidazoles which were then transformed into title compounds by treatment with nitric acid.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 1","pages":"15-28"},"PeriodicalIF":0.0,"publicationDate":"1988-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14422662","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Aromatic amidines: inhibitory effect on purified plasma serine proteinases, blood coagulation and platelet aggregation. 芳香胺类:对纯化血浆丝氨酸蛋白酶、凝血和血小板聚集的抑制作用。
Il Farmaco; edizione scientifica Pub Date : 1988-01-01
R Ferroni, E Menegatti, M Guarneri, U Taddeo, P Ascenzi, G Amiconi
{"title":"Aromatic amidines: inhibitory effect on purified plasma serine proteinases, blood coagulation and platelet aggregation.","authors":"R Ferroni,&nbsp;E Menegatti,&nbsp;M Guarneri,&nbsp;U Taddeo,&nbsp;P Ascenzi,&nbsp;G Amiconi","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The inhibitory effect of benzamidine as well as of 1,3-di-(p-amidinophenoxy)-2,2-bis-(p-amidinophenoxymethyl)propane (TAPP-H) and TAPP-halo derivatives (with Cl, Br or I) on (i) the catalytic properties of purified plasma serine proteinases (notably, factor Xa, factor VIIa, thrombin and plasmin), (ii) blood coagulation, and (iii) platelet aggregation was investigated in vitro. For all the enzyme/inhibitor systems examined, the inhibition patterns were strictly competitive, and titrations conformed to simple equilibria. The inhibitory effect of TAPP-H and TAPP-halo derivatives is higher, by at least 10-fold, than that of benzamidine, which binds at the primary specificity subsite (S1) of serine proteinases and is commonly taken as a molecular inhibitor model. The high inhibitory effect of aromatic tetraamidines has been interpreted taking into account an additional productive binding for a second benzamidine or halo-benzamidine moiety to the enzyme surface. As a whole, the data reported here indicate that aromatic amidines inhibit the plasma serine proteinases involved in different steps of haemostasis (coagulation and platelet aggregation) as well as clot lysis under physiological-like conditions in vitro.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 1","pages":"5-13"},"PeriodicalIF":0.0,"publicationDate":"1988-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14295340","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Ureas and amides derived from N-(5-norbornen-2-ylmethyl) bornan-2-exo-amine with antiarrhythmic and other activities. 由N-(5-降冰片-2-甲基)冰片-2-外显胺衍生的脲类和酰胺类，具有抗心律失常和其他活性。
Il Farmaco; edizione scientifica Pub Date : 1988-01-01
A Ranise, F Bondavalli, P Schenone, M Angrisani, M Lisa, R Marrazzo, E Marmo
{"title":"Ureas and amides derived from N-(5-norbornen-2-ylmethyl) bornan-2-exo-amine with antiarrhythmic and other activities.","authors":"A Ranise,&nbsp;F Bondavalli,&nbsp;P Schenone,&nbsp;M Angrisani,&nbsp;M Lisa,&nbsp;R Marrazzo,&nbsp;E Marmo","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis of title compounds by reaction of camphor nitrimine with (5-norbornen-2-yl)methylamine, followed by NaBH4 reduction of the resulting imine to N-substituted isobornylamine (IV) and reaction of (IV) with alkyl and aryl isocyanates or acyl chlorides, is described. Some ureas and amides are endowed with antiarrhythmic activity in rats superior or comparable to that of quinidine, whereas benzamide (V o) showed an appreciable hypoglycemic activity in mice. Moreover, compounds (V) exhibited in general moderate hypotensive, bradycardic and antiinflammatory activities in rats, as well as a weak infiltration anesthesia in mice.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 1","pages":"79-89"},"PeriodicalIF":0.0,"publicationDate":"1988-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14521131","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and dopamine receptors binding affinity of 2-(3-fluoro-4-hydroxyphenyl)ethylamine and its N-alkyl derivatives. 2-(3-氟-4-羟基苯基)乙胺及其n -烷基衍生物的合成及多巴胺受体结合亲和力。
Il Farmaco; edizione scientifica Pub Date : 1988-01-01
M Cardellini, G M Cingolani, F Claudi, V Perlini, W Balduini, F Cattabeni
{"title":"Synthesis and dopamine receptors binding affinity of 2-(3-fluoro-4-hydroxyphenyl)ethylamine and its N-alkyl derivatives.","authors":"M Cardellini,&nbsp;G M Cingolani,&nbsp;F Claudi,&nbsp;V Perlini,&nbsp;W Balduini,&nbsp;F Cattabeni","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The 2-(3-fluoro-4-hydroxyphenyl)ethylamine and its N,N-dialkyl derivatives were synthesized. The affinity of new compounds for dopamine binding sites was measured in a test involving displacement of [3H]SCH 23390 (D-1 selective) and [3H]spiperone (D-2 selective) from homogenized rat striatal tissue. No compound proved effective in displacing [3H]SCH 23390. Two derivatives are selective displacers of [3H]spiperone.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 1","pages":"49-59"},"PeriodicalIF":0.0,"publicationDate":"1988-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14035699","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and biological activity of some pyrrole derivatives. I. 一些吡咯衍生物的合成及其生物活性。我。
Il Farmaco; edizione scientifica Pub Date : 1988-01-01
M T Cocco, C Congiu, A Maccioni, A Plumitallo, M L Schivo, G Palmieri
{"title":"Synthesis and biological activity of some pyrrole derivatives. I.","authors":"M T Cocco,&nbsp;C Congiu,&nbsp;A Maccioni,&nbsp;A Plumitallo,&nbsp;M L Schivo,&nbsp;G Palmieri","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis of some 5-substituted 2-amino-3-cyano (and 3-carboethoxy)pyrroles is described starting from the cyano- and carboethoxyacetomidines and the alpha-halogeno ketones. The compounds tested in vitro as antimicrobial agents did not show any significative activity.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 1","pages":"103-12"},"PeriodicalIF":0.0,"publicationDate":"1988-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14422661","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
首页 上一页
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整，为了账户安全，请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们：info@booksci.cn Book学术提供免费学术资源搜索服务，方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号：481959085
Book学术官方微信